A Review Article on Buccal Patch

The buccal mucosa is one of the administration sites that might provide an alternative for peroral administration. The successful delivery of drugs across the oral mucosa represents a continuing challenge, as well as a great opportunity. Buccal delivery, has progressed far beyond the use of traditional dosage forms with novel approaches emerging continuously. Buccal drug delivery system in which drug enters directly in systemic circulation thereby by passing the first pass effect. This is painless and without discomfort, precise dosage form and facilitates ease of removal without significant associated pain. Moreover it shows better stability, patient compliance; uniform and sustained drug release and above all easy and cheap methods of preparation which can be done with various commonly available biocompatible polymers. The buccal route has been researched for a wide variety of drugs and has gained significant attention and momentum since it offers remarkable advantages. Over past few decades, buccal route for systemic drug delivery using mucoadhesive polymers to significantly improve the performance of many drugs has been of profound interest. Present article deals with the different aspect of the buccal patches.

Mucoadhesive buccal patches containing propranolol hydrochloride were prepared using the solvent casting method. Chitosan was used as bioadhesive polymer and different ratios of chitosan to PVP K-30 were used. The patches were evaluated for their physical characteristics like mass variation, drug content uniformity, folding endurance, ex vivo mucoadhesion strength, ex vivo mucoadhesion time, surface pH, in vitro drug release, and in vitro buccal permeation study. Patches exhibited controlled release for a period of 7 h. The mechanism of drug release was found to be non-Fickian diffusion and followed the first-order kinetics. Incorporation of PVP K-30 generally enhanced the release rate. Swelling index was proportional to the concentration of PVP K-30. Optimized patches (F4) showed satisfactory bioadhesive strength of 9.6 +/- 2.0 g, and ex vivo mucoadhesion time of 272 minutes. The surface pH of all patches was between 5.7 and 6.3 and hence patches should not cause irritation in the buccal cavity. Patches containing 10 mg of drug had higher bioadhesive strength with sustained drug release as compared to patches containing 20 mg of drug. Good correlation was observed between the in vitro drug release and in vitro drug permeation with a correlation coefficient of 0.9364. Stability study of optimized patches was done in human saliva and it was found that both drug and buccal patches were stable.

The administration of drug through buccal mucosa has gain lot of attention in drug delivery system. The main advantages of using buccal route is non-invasive and easy method to administer the drug and it bypasses the gastrointestinal tract and avoids first pass metabolism in the liver that lead to reduced side effects. However, the buccal drug delivery faces many challenges like low permeability, enzyme degradation and drug absorption typically inadequate to provide effective therapy because of tongue movement, high salivary excretion and accidental swallowing. The use of nanoparticle is a key method for improving buccal administration because the nanoparticle act as versatile nanocarriers than can increase the bioavailability of loaded drug and improve permeability and drug absorption in buccal mucosa since they can stay in systemic circulation for long period of time and reduce side effects. Many drugs have been formulated as nanoparticle based buccal delivery system such as lipid-based nanoparticle, liposomes, nanoparticle lipid carriers, polymerics, etc., which are used in the treatment of various diseases. This review article highlights the buccal drug delivery, anatomy of oral cavity and various strategies used to target the buccal mucosa. Also, this review summarizes the recent advance nanotechnology method focused on formulations that have been developed to enhance drug delivery through buccal mucosa.

5 - Composites of hydrogels and nanoparticles: A potential solution to current challenges in buccal drug delivery

The present review aims to enlighten about a potential dosage form that is mouth dissolving films. Mouth dissolving film is a rapidly dissolving dosage form that dissolves in the mouth within a few seconds without the intake of water and is mainly used for pediatric and geriatric patients due to its flexibility and patient compliance. It is a potential dosage form for drugs having high metabolism and low bioavailability. Solvent casting, hot melt extrusion, solid dispersion, semisolid casting, rolling, and other processes can all be used to create mouth dissolving film, but solvent casting is the most popular due to its consistency and superior physical properties. Mouth dissolving film is evaluated for the following parameters like physical parameters and chemical parameters. The review sums up information on drug delivery by mouth dissolving films as a promising dosage form for delivering drugs to children and elderly patients, as well as information on its formulation considerations, preparation process, and evaluation criteria. Keywords: Mouth dissolving film, Buccal film, Improved patient compliance, Standard composition, Method of preparation, Evaluation

Chapter 8 - (Trans)buccal drug delivery

The eye is God's most wonderful creation of all the sense organs in the human body since it allows us to see numerous objects both near and far away. An ocular implant is a cutting-edge device for treating eye diseases. The design and development of an ocular insert has always been a difficulty for pharmaceutical researchers and manufacturers. Ocuserts, also known as ophthalmic inserts, are "sterile preparations in the form of solid or semisolid, whose size and shape are specially designed to be applied to the eyes". Solvent casting, the Glass Substrate technique, and hot melt extrusion were used to create ocuserts. The inserts can be classed as insoluble, soluble, or biodegradable based on their solubility. The drug's release from the insert is determined by its diffusion, osmosis, and bioerosion. The ocuserts' objective is to enhance pharmaceutical contact with conjunctiva tissue, resulting in constant dose release. Uniform ocular drug levels reduce systemic side effects, minimise doses, and improve patient compliance. Preparing ocular inserts aims to enhance medication bioavailability. Ocular inserts keep medication concentrations within the appropriate range. Using fewer administrations leads to better patient compliance. The page covers the eye's many parts and anatomy, along with an explanatory image.This study aims to offer an update on current understanding in ocular medication delivery. Also, this review focuses on the current usage of ocuserts to treat eye disorders.

Purpose: To develop mucoadhesive patches for buccal administration of metoprolol succinate and to evaluate their in vitro and in vivo bioadhesion.Methods: The mucoadhesive buccal patches were prepared by solvent casting technique using two different mucoadhesive polymers. The formulations were tested for in vitro drug permeation studies, buccal absorption, in vitro drug release studies, moisture absorption as well as for in vitro and in vivo bioadhesion.Results: The peak detachment force and work of adhesion for MC5 (sodium carboxymethylcellulose, i.e., Na CMC) patch were 0.87 N and 0.451 mJ respectively and the corresponding values for CH5 (chitosan) were 5.15N and 0.987 mJ. Formulation CH5 (prepared with chitosan) showed 67.1 % release, while MC5 (Na CMC) showed drug release of 81.9 % in 6 h. Basic pharmacokinetic parameters such as Cmax, Tmax and AUCtotal varied statistically (p < 0.05) when given by the buccal route compared with that of the solution given by the oral route.Conclusion: The results indicate that formulation of suitable bioadhesive buccal patches with the desired permeability is feasible. The development of bioadhesive buccal formulation for metoprolol succinate with a lower dose and few side effects may be attainable.Keywords: Mucoadhesive, Buccal patches, Metoprolol succinate, Sodium carboxymethylcellulose, Chitosan, Bioavailability

An overview of polymeric dosage forms in buccal drug delivery: State of art, design of formulations and their in vivo performance evaluation

The existence of 3D printing (3DP) ways back to 1992, and its sound presence in the pharmaceutical industry was made in 2015 by the launch of 1st 3D printed drug, Spritam was manufactured by Aprecia Pharmaceuticals. Implementation of 3DP is escalating in the number of industries, including the pharmaceutical industry. The purpose of this review paper is to briefly discuss types of 3DP and their role in formulating novel dosage forms. Binder jet printing, VAT polymerization, powder bed fusion, and material extrusion are briefly explained along with an example of their implementation in the formulation of the dosage form. A few novel dosage forms which can bypass the first-pass metabolism and how 3D printing is useful in formulating them as been discussed. It also includes a comparison of the process of 3D printed tablets and conventional methods of manufacturing. The significance of 3D printing in novel dosage form and augmenting 3DP with hot-melt extrusion (HME) method is discussed. The regulatory concerns in adopting this technology on a large-scale are addressed. 3DP technology could rapidly print transdermal needles, buccal patches, and different shapes of vaginal rings and proved it can be a versatile tool in formulation technology. As the pharmaceutical industry involves stringent regulations, certain aspects need to be considered by regulatory authorities before implementing this tool into commercialscale manufacturing.

It is well known that certain medications suffer hepatic first-pass metabolism or deteriorate in the digestive system, the buccal drug delivery method may be an alternative to oral administration. Because it is painless and may be swiftly and readily removed if the treatment must be terminated or interrupted, the buccal mucosa has long been ideal for administering medications. This paper focuses on the buccal drug delivery system had the goal of gathering recent literature and presenting a concise explanation of buccal patches by discussing the characteristics of an ideal mucoadhesive system, benefits of buccal delivery and disadvantages thereof, factors affecting buccal absorption, and various types of patches as well as the preparation method and composition thereof. The compilation of the data is also enhanced by adding market products as well as the patented, so that reader will get the complete knowledge about the buccal drug delivery.

Polysaccharide-based micro/nanohydrogels for delivering macromolecular therapeutics.

Microparticulate drug delivery system (MDDS) has attained much consideration in the modern era due to its effectiveness in overcoming traditional treatment problems. Microparticles (MPs) are spherical particles of a diameter ranging from 10 μm to 1000 μm. MPs can encapsulate both water-soluble and insoluble compounds. MDDS proved their efficacy in improving drugs bioavailability, stability, targeting, and controlling their release patterns. MPs also offer comfort, easy administration, and improvement in patient compliance by reducing drugs toxicity and dosage frequency. This review elucidates the fabrication techniques, drug release, and therapeutic application of MDDS. Further details concerning the therapeutic applications of antidiabetic drugs-loaded MPs were also reviewed, including controlling drugs release by gastroretention, improving drugs dissolution, reducing side effects, localizing drugs to the site of disease, improving insulin stability, natural products loaded with MPs, sustained drug release, mucosal delivery, and administration routes. Additionally, the current situation and future prospects in developing MPs loaded with antidiabetic drugs were discussed.

Rheumatoid arthritis (RA) is a long-term inflammatory disease that causes synovial joint inflammation, which causes pain, stiffness, and gradual joint destruction. In addition to having a major effect on quality of life, the illness may result in systemic problems. The goal of current treatment approaches, which include biologics, corticosteroids, disease-modifying antirheumatic medications (DMARDs), and nonsteroidal anti-inflammatory medicines (NSAIDs), is to manage symptoms and halt the course of the disease. These treatments, however, frequently have problems like poor effectiveness, systemic side effects, and exorbitant expenses. Advanced, tailored medication delivery methods like nanocarriers are necessary because managing RA is made more difficult by poor patient adherence and limited targeting of inflammatory areas. Berberine and curcumin are bioactive natural compounds with significant therapeutic potential, particularly in managing inflammatory and autoimmune conditions like rheumatoid arthritis (RA). Berberine exhibits potent anti-inflammatory, immunomodulatory, and antioxidant properties, effectively suppressing pro-inflammatory cytokines and oxidative stress Curcumin, a polyphenol derived from turmeric, also demonstrates strong anti-inflammatory and antioxidant effects, inhibiting key molecular pathways involved in RA pathogenesis, such as NF-κB activation. Despite their promising pharmacological profiles, both compounds face challenges like poor water solubility, low bioavailability, and rapid metabolism. Advanced drug delivery systems, such as nanostructured lipid carriers, offer a solution to enhance their therapeutic efficacy and clinical applicability. Nanostructured lipid carriers (NLCs) are advanced drug delivery systems offering numerous advantages for therapeutic applications. Their unique structure, combining solid and liquid lipids, enhances drug solubility, stability, and bioavailability. NLCs enable controlled and sustained drug release, reducing dosing frequency and improving patient compliance. They can protect sensitive drugs like berberine and curcumin from degradation, extending their shelf life. Additionally, NLCs can be functionalized for targeted delivery, increasing drug accumulation at inflamed joints in conditions like rheumatoid arthritis while minimizing systemic side effects. Their biocompatibility and scalability make NLCs a promising platform for improving the clinical efficacy of challenging therapeutic agents. Berberine and curcumin exhibit remarkable anti-inflammatory and antioxidant properties, making them promising candidates for managing rheumatoid arthritis (RA). However, their clinical potential is limited by poor solubility and bioavailability. Nanostructured lipid carriers (NLCs) address these limitations by enhancing drug stability, targeted delivery, and controlled release. Preclinical studies demonstrate improved therapeutic efficacy of NLC formulations in RA models, though clinical translation remains limited. Future research should focus on optimizing NLC designs for enhanced targeting, scalability, and regulatory compliance. Combining these carriers with advanced therapeutic strategies offers a pathway to more effective and patient-friendly RA treatments, bridging lab discoveries to clinical practice

Locoregional drug delivery is a novel approach for the effective delivery of anti-cancer agents as it exposes the tumors to high concentration of drugs. In situ gelling systems have fetched paramount attention in the field of localized cancer chemotherapy due to their targeted delivery, ease of preparation, prolonged or sustained drug release and improved patient compliance. Numerous polymers have been investigated for their properties like swelling along with biodegradation, drug release and physicochemical properties for successful targeting of the drugs at the site of implantation. The polymers such as chitosan, Hyaluronic Acid (HA), poloxamer, Poly Glycolic Lactic Acid (PGLA) and Poly Lactic Acid (PLA) tend to form in situ hydrogels and have been exploited to develop localized delivery vehicles. These formulations are administered in the solution form and on exposure to physiological environment such as temperature, pH or ionic composition they undergo phase conversion into a hydrogel drug depot. The use of in situ gelling approach has provided prospects to increase overall survival and life quality of cancer patient by enhancing the bioavailability of drug to the site of tumor by minimizing the exposure to normal cells and alleviating systemic side effects. Because of its favorable safety profile and clinical benefits, United States Food and Drug Administration (U.S. FDA) has approved polymer based in situ systems for prolonged locoregional activity. This article discusses the rationale for developing in situ systems for targeted delivery of anti-cancer agents with special emphasis on types of polymers used to formulate the in situ system. In situ formulations for locoregional anti-cancer drug delivery that are marketed and are under clinical trials have also been discussed in detail in this article.